Giełdanowski J, Kowalczyk-Bronisz S H
Arch Immunol Ther Exp (Warsz). 1978;26(1-6):921-9.
37 newly synthesized compounds in the group of thiazoloacetic and thiazinocarboxyl aciderivatives with the possibly immunotropic, antiinflammatory and probably central activity were studied. A number of them was not resorbed and only 21 agents were immunopharmacologically investigated. The correlations between the biological activity and chemical structure were confirmed. Among acyl derivatives of thiazoloacetic acid the compounds containing two carboxyl radicals at C2 and C5 revealed the most interesting activity. For 2-N-aralkylo-alfa-sulfonic derivatives of thiazoloacetic acid, the distinct immunosuppressive activity with antiinflammatory component was found. The group of 16 derivatives of thiazinocarboxyl acid had the chemical structure correlated with the immunotropic activity (immunosuppressive or immunostimulative) and antiinflammatory component. Immunosuppressive activity was manifested, in the first place, by the derivatives containing radicals--ethyl, butyl, methoxyphenyl and two groups of cyclohexyl. The compound with allylimino group showed, however, the most immunostimulating activity. The antiinflammatory activity was correlated especially with radicals--cyclohexyl, chlorophenyl and allylimino.
对37种新合成的噻唑并乙酸和噻嗪羧酸衍生物进行了研究，这些衍生物可能具有免疫调节、抗炎以及可能的中枢活性。其中许多化合物无法被吸收，仅对21种药物进行了免疫药理学研究。证实了生物活性与化学结构之间的相关性。在噻唑并乙酸的酰基衍生物中，在C2和C5处含有两个羧基的化合物表现出最有趣的活性。对于噻唑并乙酸的2-N-芳烷基-α-磺酸衍生物，发现了具有抗炎成分的明显免疫抑制活性。16种噻嗪羧酸衍生物的化学结构与免疫调节活性（免疫抑制或免疫刺激）以及抗炎成分相关。免疫抑制活性首先表现为含有乙基、丁基、甲氧基苯基和两组环己基基团的衍生物。然而，含有烯丙基亚氨基的化合物表现出最强的免疫刺激活性。抗炎活性尤其与环己基、氯苯基和烯丙基亚氨基基团相关。
